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Arylmethoxypyridines as novel, potent and orally active mGlu5 receptor antagonists.
Büttelmann B, Peters JU, Ceccarelli S, Kolczewski S, Vieira E, Prinssen EP, Spooren W, Schuler F, Huwyler J, Porter RH, Jaeschke G. Büttelmann B, et al. Among authors: porter rh. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1892-7. doi: 10.1016/j.bmcl.2005.12.088. Epub 2006 Jan 24. Bioorg Med Chem Lett. 2006. PMID: 16439120
Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases.
Jaeschke G, Kolczewski S, Spooren W, Vieira E, Bitter-Stoll N, Boissin P, Borroni E, Büttelmann B, Ceccarelli S, Clemann N, David B, Funk C, Guba W, Harrison A, Hartung T, Honer M, Huwyler J, Kuratli M, Niederhauser U, Pähler A, Peters JU, Petersen A, Prinssen E, Ricci A, Rueher D, Rueher M, Schneider M, Spurr P, Stoll T, Tännler D, Wichmann J, Porter RH, Wettstein JG, Lindemann L. Jaeschke G, et al. Among authors: porter rh. J Med Chem. 2015 Feb 12;58(3):1358-71. doi: 10.1021/jm501642c. Epub 2015 Feb 2. J Med Chem. 2015. PMID: 25565255
Synthesis and biological evaluation of fenobam analogs as mGlu5 receptor antagonists.
Jaeschke G, Porter R, Büttelmann B, Ceccarelli SM, Guba W, Kuhn B, Kolczewski S, Huwyler J, Mutel V, Peters JU, Ballard T, Prinssen E, Vieira E, Wichmann J, Spooren W. Jaeschke G, et al. Bioorg Med Chem Lett. 2007 Mar 1;17(5):1307-11. doi: 10.1016/j.bmcl.2006.12.033. Epub 2006 Dec 15. Bioorg Med Chem Lett. 2007. PMID: 17196387
CTEP: a novel, potent, long-acting, and orally bioavailable metabotropic glutamate receptor 5 inhibitor.
Lindemann L, Jaeschke G, Michalon A, Vieira E, Honer M, Spooren W, Porter R, Hartung T, Kolczewski S, Büttelmann B, Flament C, Diener C, Fischer C, Gatti S, Prinssen EP, Parrott N, Hoffmann G, Wettstein JG. Lindemann L, et al. J Pharmacol Exp Ther. 2011 Nov;339(2):474-86. doi: 10.1124/jpet.111.185660. Epub 2011 Aug 17. J Pharmacol Exp Ther. 2011. PMID: 21849627
Metabolite identification via LC-SPE-NMR-MS of the in vitro biooxidation products of a lead mGlu5 allosteric antagonist and impact on the improvement of metabolic stability in the series.
Ceccarelli SM, Schlotterbeck G, Boissin P, Binder M, Buettelmann B, Hanlon S, Jaeschke G, Kolczewski S, Kupfer E, Peters JU, Porter RH, Prinssen EP, Rueher M, Ruf I, Spooren W, Stämpfli A, Vieira E. Ceccarelli SM, et al. Among authors: porter rh. ChemMedChem. 2008 Jan;3(1):136-44. doi: 10.1002/cmdc.200700203. ChemMedChem. 2008. PMID: 17994660
Fenobam: a clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activity.
Porter RH, Jaeschke G, Spooren W, Ballard TM, Büttelmann B, Kolczewski S, Peters JU, Prinssen E, Wichmann J, Vieira E, Mühlemann A, Gatti S, Mutel V, Malherbe P. Porter RH, et al. J Pharmacol Exp Ther. 2005 Nov;315(2):711-21. doi: 10.1124/jpet.105.089839. Epub 2005 Jul 22. J Pharmacol Exp Ther. 2005. PMID: 16040814
Pharmacology of basimglurant (RO4917523, RG7090), a unique metabotropic glutamate receptor 5 negative allosteric modulator in clinical development for depression.
Lindemann L, Porter RH, Scharf SH, Kuennecke B, Bruns A, von Kienlin M, Harrison AC, Paehler A, Funk C, Gloge A, Schneider M, Parrott NJ, Polonchuk L, Niederhauser U, Morairty SR, Kilduff TS, Vieira E, Kolczewski S, Wichmann J, Hartung T, Honer M, Borroni E, Moreau JL, Prinssen E, Spooren W, Wettstein JG, Jaeschke G. Lindemann L, et al. Among authors: porter rh. J Pharmacol Exp Ther. 2015 Apr;353(1):213-33. doi: 10.1124/jpet.114.222463. Epub 2015 Feb 9. J Pharmacol Exp Ther. 2015. PMID: 25665805
Comparison of the binding pockets of two chemically unrelated allosteric antagonists of the mGlu5 receptor and identification of crucial residues involved in the inverse agonism of MPEP.
Malherbe P, Kratochwil N, Mühlemann A, Zenner MT, Fischer C, Stahl M, Gerber PR, Jaeschke G, Porter RH. Malherbe P, et al. Among authors: porter rh. J Neurochem. 2006 Jul;98(2):601-15. doi: 10.1111/j.1471-4159.2006.03886.x. J Neurochem. 2006. PMID: 16805850 Free article.
123 results